TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
TC-MCH 7c has an IC50 of 9.7 μM for MCH1R in [Ca]i mobilization.
TC-MCH 7c has IC50s of 23 nM and 9.0 μM for FLIPR and hERG, respectively.
体内研究
TC-MCH 7c (oral; 3-30 mg/kg; once-daily for 1.5 months) exhibits excellent body weight reduction in a dose-dependent manner in DIO mice model.
TC-MCH 7c (oral; 3-30 mg/kg) with 30 mg/kg has plasma concentrations of 5.1, 1.8, and 0.7 μM at 2, 15, and 24 hours, respectively.
Animal Model:
C57BL/6J DIO mice
Dosage:
3, 10 and 30 mg/kg
Administration:
Oral; once-daily for 1.5 months
Result:
Exhibited excellent body weight reduction in a dose-dependent manner.
Animal Model:
Diet-induced obesity mice
Dosage:
3, 10 and 30 mg/kg (Pharmacokinetic Analysis)
Administration:
Oral
Result:
Plasma concentrations at 2, 15, and 24 hours were 5.1, 1.8, and 0.7 μM, respectively.
分子式
C24H25FN2O3
分子量
408.47
CAS号
864756-35-4
运输条件
Room temperature in continental US; may vary elsewhere.